526561
PI 3-K/mTOR Inhibitor III, PKI-179
The PI 3-K/mTOR Inhibitor III, PKI-179, also referenced under CAS 1197160-28-3, controls the biological activity of PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
同義詞:
PI 3-K/mTOR Inhibitor III, PKI-179
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About This Item
推薦產品
品質等級
化驗
≥98% (HPLC)
形狀
solid
製造商/商標名
Calbiochem®
儲存條件
OK to freeze
desiccated (hygroscopic)
protect from light
顏色
white
溶解度
DMSO: 50 mg/mL
運輸包裝
ambient
儲存溫度
2-8°C
SMILES 字串
O=C(NC1=CC=NC=C1)NC2=CC=C(C=C2)C3=NC(N4[C@H]5COC[C@@H]4CC5)=NC(N6CCOCC6)=N3.[xH2O]
InChI
1S/C25H28N8O3/c34-25(28-19-7-9-26-10-8-19)27-18-3-1-17(2-4-18)22-29-23(32-11-13-35-14-12-32)31-24(30-22)33-20-5-6-21(33)16-36-15-20/h1-4,7-10,20-21H,5-6,11-16H2,(H2,26,27,28,34)
InChI 密鑰
WXUUCRLKXQMWRY-UHFFFAOYSA-N
一般說明
A cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR (IC50 = 0.42 nM) and PI 3-K (IC50 = 8, 24, 74, 77, 14, and 11 nM against isoform α, β, γ, δ, α E545K mutant, and α H1047R mutant, respectively) activities, exhibiting much reduced or little activity against a panel of 361 other kinases (IC50 >50 µM), Cytochrome CYP isoforms, or hERG. It is reported to be orally available in mouse, rat, monkey, and dog species, and effectively suppress cancer growth both in cultures in vitro (IC50 = 22 and 29 nM, respectively, against MDA361 and PC3mm2) and in mice in vivo (by 30% of control MDA361 tumor size on day 42; 50 mg/kg/day p.o.) via apoptosis induction as a result of Akt/mTOR pathway inhibition.
A cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR and PI 3-K activities (IC50 = 0.42 nM against mTOR; IC50 = 8, 24, 74, 77, 14, and 11 nM against PI 3-K isoform α, β, γ, δ, α E545K mutant, and α H1047R mutant, respectively), exhibiting much reduced potency against Cytochrome CYP 2C8 (IC50 = 3 µM) and little or no activity toward 7 other Cytochrome CYP isoforms, hERG (IC50 >30 µM) and a panel of 361 other kinases (IC50 >50 µM). It is reported to be orally available in mouse, rat, monkey, and dog (bioavailability = 98%, 46%, 38%, and 61%, respectively; 10 mg/kg), and effectively suppress cancer growth both in cultures in vitro (IC50 = 22 and 29 nM, respectively, against MDA361 and PC3mm2) and in mice in vivo (40% and 30% of control MDA361 tumor size on day 42, respectively, via daily p.o. dosage of 10 mg/kg and 50 mg/kg) via apoptosis induction as a result of Akt/mTOR pathway inhibition. Although liver microsome stability data indicate a much faster compound metabolism in human (t1/>> = 14 min) and monkey than in mouse, rat (t1/>> >30 min), and dog, the major metabolite remains biologically potent against kinase targets (IC50 =0.8, 4, and 33 nM against mTOR, PI 3-Kα, and PI 3-γ, respectively) and cancer cell proliferation (IC50 = 32 and 80 nM, respectively, against MDA361 and PC3mm2).
The PI 3-K/mTOR Inhibitor III, PKI-179, also referenced under CAS 1197160-28-3, controls the biological activity of PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
包裝
Packaged under inert gas
警告
Toxicity: Regulatory Review (Z)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他說明
Venkatesan, A.M., et al. 2010. Bioorg. Med. Chem. Lett.20, 5869.
Chen, Z., et al. 2010. J. Org. Chem.75, 1643.
Chen, Z., et al. 2010. J. Org. Chem.75, 1643.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
分析證明 (COA)
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